In recent years, a series of radioactive halogen-labeled amino acid compounds including [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F]-FACBC) have been designed as novel radiopharmaceuticals. [18F]-FACBC is considered to be effective as a diagnostic agent for highly proliferative tumors, because it has a property of being taken up specifically by amino acid transporters on the tumors.
Though there are a number of published approaches for the synthesis of [18F]-FACBC and its precursors, some suffer from being lengthy (e.g., EP1978015), low yields or from problems associated with the purification of either the final product (i.e., [18F]-FACBC) and/or the intermediates leading to the production of the product. Accordingly, there remains a need for new methods for the production of [18F]-FACBC and/or intermediates leading to the production of [18F]-FACBC.